Effect of concentration, pH, and preservative on in vitro transcorneal permeation of ibuprofen and flurbiprofen from non-buffered aqueous drops.
Influence of drug concentration, pH of aqueous drops and some commonly used preservatives on in vitro transcorneal permeation of ibuprofen and flurbiprofen were investigated using goat cornea. Increase in drug concentration in the drops made in normal saline resulted in increase in quantity permeated but decrease in cumulative percent permeation of both drugs. Permeation of each drug from 0.5% drops was maximum at acidic pH (6.4) and decreased with increase in pH of the drops. Normal saline, as a vehicle, favoured permeation of each drug, hence retained in the formulation. Benzalkonium chloride and chlorobutanol enhanced cumulative percent permeation of ibuprofen while benzalkonium chloride and phenyl mercuric nitrate increased permeation of flurbiprofen. Benzalkonium chloride being incompatible with 0.5% drops (pH 6.4) of either drug, chlorobutanol appears suitable for ibuprofen drops and phenyl mercuric nitrate for flurbiprofen drops.
Gupta
M
M
College of Pharmacy (University of Delhi), India.
Majumdar
D K
DK
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000493:pharmacokinetics*; D002021:Buffers; D003315:Cornea / Q000378:metabolism*; D005480:Flurbiprofen / Q000493:pharmacokinetics*; D006041:Goats / Q000378:metabolism*; D006863:Hydrogen-Ion Concentration; D007052:Ibuprofen / Q000493:pharmacokinetics*; D009883:Ophthalmic Solutions / Q000378:metabolism*; D010539:Permeability; D011310:Preservatives, Pharmaceutical; D014867:Water
D000894:Anti-Inflammatory Agents, Non-Steroidal; D002021:Buffers; D009883:Ophthalmic Solutions; D011310:Preservatives, Pharmaceutical; D014867:Water; D005480:Flurbiprofen; D007052:Ibuprofen